Toxicological and local anaesthetic effects of optically active isomers of two local anaesthetic compounds.
Toxicological and local anaesthetic effects of optically active isomers of two local anaesthetic compounds.
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两种局部麻醉化合物的光学活性异构体的毒理学和局部麻醉作用。
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发表时间：
1972
期刊：
影响因子：
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通讯作者：
G. Åberg
中科院分区：
文献类型：
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作者：
G. Åberg
甲哌卡因：甲哌卡因的两种旋光异构体快速静脉注射给小鼠或大鼠后，毒性没有差异。然而，缓慢静脉注射或皮下注射后，L(+)-异构体的毒性低于D(-)-异构体。这至少可以部分地通过其他实验获得的结果来解释，这些实验表明，在向兔子缓慢输注药物后，肺部吸收的 L(+)-甲哌卡因多于 D(-)-甲哌卡因，从而降低了到达大脑的药物浓度，在大脑中发现 D(-)-甲哌卡因明显多于 L(+)-甲哌卡因。与D(-)-甲哌卡因相比，L(+)-甲哌卡因在注射部位的吸收较慢，这可能是导致皮下毒性差异的原因，也可能是L(+)-异构体的浸润麻醉持续时间明显长于D(-)-异构体的原因，因为在体外发现了异构体相同的神经阻滞作用。布比卡因：布比卡因异构体静脉注射和皮下注射时的毒性存在显着差异； D(+)-异构体毒性更大。这以及 L(-)-布比卡因的浸润麻醉持续时间非常长，表明布比卡因异构体之间的吸收率差异与甲哌卡因异构体的吸收率相似。
Mepivacaine: There was no difference in toxicity between the two optical isomers of mepivacaine after rapid intravenous injections into mice or rats. After slow intravenous injections or after subcutaneous injections the L(+)– isomer however was less toxic than the D(-) – isomer. This might at least partly be explained by the results obtained from other experiments, which demonstrated that after slow infusions of the drugs into rabbits more L(+)–mepivacaine than D(-)–mepivacaine was taken up by the lungs, thus reducing the concentration of the drug reaching the brain, where significantly more D(-)– mepivacaine than L(+)–mepivacaine was found. A slow absorption of L(+)–mepivacaine in comparison with D(-)–mepivacaine from the site of injection is demonstrated and might contribute to the differences in subcutaneous toxicity and might also be the cause of the significantly longer duration of infiltration anaesthesia by the L(+)–isomer than by the D(-)–isomer, since the same nerve-blocking effect of the isomers was found in vitro. Bupivacaine: There were significant differences between the toxicity of the bupivacaine isomers when given intravenously and subcutaneously; the D(+)–isomer was more toxic. This as well as the very long duration of infiltration anaesthesia by L(-)–bupivacaine indicate differences in absorption rates between the bupivacaine isomers similar to those demonstrated for the mepivacaine isomers.